Dimethylenastron
Based on 4 publication(s) in Google Scholar
Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC50 of 200 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.27%
- No. CAS: 863774-58-7
- Fòrmula: C16H18N2O2S
- Peso molecular:302.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Dimethylenastron
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In Vivo Efficacy Study
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Histological Imaging/Staining
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IF
Ver todos los productos específicos de isoformas Kinesin
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Actividad biológica
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Eg5 200 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | EC50 |
743 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
| HCT-116 | EC50 |
330 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
| K562 | EC50 |
769 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
| KB 3-1 | EC50 |
594 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay in presence of zosuquidar
Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay in presence of zosuquidar
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[PMID: 20597485] |
| KB 3-1 | EC50 |
661 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
| KB-V1 | EC50 |
12303 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay
Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
| KB-V1 | EC50 |
434 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar
Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar
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[PMID: 20597485] |
| NCI-H1299 | EC50 |
881 nM
Compound: rac-dimethylenastron
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Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
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[PMID: 20597485] |
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM. Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells[1]. Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 863774-58-7
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Appearance Solid
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Peso molecular 302.39
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Fòrmula C16H18N2O2S
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Color White to off-white
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SMILES
O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Kinesin-5 Eg5 is essential for spindle assembly, chromosome stability and organogenesis in development. [Abstract]2022 Dec 13;8(1):490. PMID: 36513626
Dimethylenastron purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Dec 13;8(1):490. [Abstract]
Mouse body weight in the control, STLC, and Dimethylenastron (3 mg/kg, i.p.) groups were shown.
Dimethylenastron purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Dec 13;8(1):490. [Abstract]
Representative HE staining of mouse spleen in the DMSO, STLC, and Dimethylenastron (3 mg/kg, i.p.) groups.
Dimethylenastron purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Dec 13;8(1):490. [Abstract]
Representative immunofluorescence images of Eg5 and α-tubulin. DAPI, blue; Eg5, green; α-tubulin, red. NIH/3T3 cells were incubated with STLC and Dimethylenastron (3 mg/kg, i.p.) for 48 h.
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Exp Cell Res
Loss-of-function of kinesin-5 KIF11 causes microcephaly, chorioretinopathy, and developmental disorders through chromosome instability and cell cycle arrest. [Abstract]2024 Mar 1;436(1):113975. PMID: 38367657 -
bioRxiv
2025 Apr 9:2023.09.04.556218. PMID: 39071426
Solvente y solubilidad
DMSO : 100 mg/mL (330.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell invasion in response to Dimethylenastron is carried out by transwell assays. The upper surface of the transwell filters is coated with matrigel or fibronectin. Cells suspended in 200 μL serum-free media are added to the chamber, and the chamber is placed in a 24-well plate containing complete medium. After 24 h of incubation at 37°C, the filters are gently taken out and matrigel on the upper surface of the filters is removed by cotton swabs. Cells on the underside of transwell filters are fixed with 4% paraformaldehyde for 30 min, stained with 0.1% crystal violet for 10 min, and then photographed. For quantitative assessment, the number of invading cells is counted in five random fields per filter. The extent of cell invasion is quantified as the number of invading cells in the drug-treatment group divided by the number of invading cells in the control group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Just after the conjunctival suture is closed, a metallic needle (30 G) is inserted into the subconjunctival space at the nasal margin of the superior rectus muscle and injection of one of the following agents is delivered: The rabbits receive either no adjuvant after the surgery in the control group, one unilateral subconjunctival injection of Dimethylenastron (1.0 µmol, 3.0 µmol) or of the vehicle (DMSO, 99.9%, 10 mg/mL) alone at baseline, which means an injection directly after surgery and in two further groups additionally at days 3 and 7 thereafter (1.0 µmol, 3.0 µmol)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7. [Content Brief]
[2]. Sun XD, et al. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8. [Content Brief]
[3]. Lüke J, et al. The effect of adjuvant dimethylenastron, a mitotic Kinesin Eg5 inhibitor, in experimental glaucoma filtration surgery. Curr Eye Res. 2010 Dec;35(12):1090-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3070 mL | 16.5349 mL | 33.0699 mL | 82.6747 mL |
| 5 mM | 0.6614 mL | 3.3070 mL | 6.6140 mL | 16.5349 mL | |
| 10 mM | 0.3307 mL | 1.6535 mL | 3.3070 mL | 8.2675 mL | |
| 15 mM | 0.2205 mL | 1.1023 mL | 2.2047 mL | 5.5116 mL | |
| 20 mM | 0.1653 mL | 0.8267 mL | 1.6535 mL | 4.1337 mL | |
| 25 mM | 0.1323 mL | 0.6614 mL | 1.3228 mL | 3.3070 mL | |
| 30 mM | 0.1102 mL | 0.5512 mL | 1.1023 mL | 2.7558 mL | |
| 40 mM | 0.0827 mL | 0.4134 mL | 0.8267 mL | 2.0669 mL | |
| 50 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.6535 mL | |
| 60 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3779 mL | |
| 80 mM | 0.0413 mL | 0.2067 mL | 0.4134 mL | 1.0334 mL | |
| 100 mM | 0.0331 mL | 0.1653 mL | 0.3307 mL | 0.8267 mL |
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